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The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus |
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| Authors: | Jeffrey A. Pfefferkorn Meihua Tu Kevin J. Filipski Angel Guzman-Perez Jianwei Bian Gary E. Aspnes Matthew F. Sammons Wei Song Jian-Cheng Li Christopher S. Jones Leena Patel Tim Rasmusson Dongxiang Zeng Kapil Karki Michael Hamilton Richard Hank Karen Atkinson John Litchfield Robert Aiello Levenia Baker Alan Robertson |
| Affiliation: | 1. Pfizer Cardiovascular, Metabolic and Endocrine Disease Research Unit, Pfizer Worldwide Research and Development, 620 Memorial Drive, Cambridge, MA 02139, USA;2. Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06442, USA |
| Abstract: | Glucokinase activators represent a promising potential treatment for patients with Type 2 diabetes. Herein, we report the identification and optimization of a series of novel indazole and pyrazolopyridine based activators leading to the identification of 4-(6-(azetidine-1-carbonyl)-5-fluoropyridin-3-yloxy)-2-ethyl-N-(5-methylpyrazin-2-yl)-2H-indazole-6-carboxamide (42) as a potent activator with favorable preclinical pharmacokinetic properties and in vivo efficacy. |
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